JNJ-39758979

Orthosteric of HRH4

Structure

SERP Rating

Probe JNJ-39758979 is in the process of SERP review.

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Information

HRH4

Orthosteric

up to 10 µM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: Q9H3N8

Target Class: GPCR

Target SubClass: Histamine Receptor

Potency: Ki

Potency Value: 12.5 nM

Potency Assay: Binding assay with membranes from cells transfected with the receptor

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Histamine H4 receptor, GPCR105, HRH4, HRH4_HUMAN, ...

DOI Reference: 10.1021/jm401727m

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: Binding assay: >50-fold selectivity vs. HRH3 (Ki 1023 nM), HRH2 (Ki > 1 µM), HRH1 (Ki > 1 µM). Selectivity outside target family: Kinase panel (66 kinases at 10 µM): clean. CEREP panel (50 targets at 1 µM) with closest off-targets: CHRM1, CHRM2, CHRM3, CHRM4 (Ki > 10 µM)

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